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Selexipag

Selexipag structure

CAS No:
475086-01-2
Formula:
C26H32N4O4S
Chemical Name:
Selexipag
Synonyms:
Selexipag;ACT-293987;NS-304(Selexipag);Selexipag API;2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylaMino]butoxy]-N-MethylsulfonylacetaMide;AcetaMide, 2-[4-[(5,6-diphenyl-2-pyrazinyl)(1-Methylethyl)aMino]butoxy]-N- (Methylsulfonyl)-;Slipper;Selexipag intermediate 1
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Selexipag and its active metabolite, the corresponding carboxylic acid, are nonprostanoid prostaglandin I2 (PGI-2) receptor agonists. The N-methylsulfonamide within selexipag is hydrolyzed to the corresponding carboxylic acid in vivo by hepatic microsomes at a rate which provides a slow-release pharmacological effect. The compound was originally discovered by Nippon Shinyaki and later licensed to Actelion for development. The drug was approved in 2015 and first launched for the oral treatment of pulmonary arterial hypertension (PAH) in the U.S. in 2016 to delay disease progression and reduce the risk of hospitalization.

ChEBI: Selexipag is a member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid). It has a role as an orphan drug, a prostacyclin receptor agonist, a platelet aggregation inhibitor, a vasodilator agent and a prodrug. It is a monocarboxylic acid amide, an ether, a member of pyrazines, an aromatic amine, a tertiary amino compound and a N-sulfonylcarboxamide. It is functionally related to an ACT-333679.

Selexipag Basic Attributes

Molecular Weight：

496.62

Exact Mass：

496.62

Color/Form：

Pale Yellow

Characteristics

Density：

1.210±0.06 g/cm3(Predicted)

Melting Point：

134-138°C

PKA：

3.82±0.40(Predicted)

Critical Temperature & Pressure：

-20°C Freezer

Safety Information

wgk germany：

WGK 3

Storage features：

Store at -20°C

Selexipag Use and Manufacturing

Selexipag is an orally available, highly selective, long-acting prostacyclin (IP) receptor agonist prodrug. It is a potential drug for the treatment of various vascular disorders such as pulmonary arterial hypertension and arteriosclerosis obliterans.

Drug Function and Efficacy

Selexipag is an oral prostacyclin receptor (IP receptor) agonist, which is structurally different from prostacyclin and is hydrolyzed by carboxylesterase 1 into an active metabolite, which is about 37 times more potent than selexipag. Selexipag and its active metabolites selectively act on IP receptors but have no effect on other prostaglandin receptors (EP, DP, FP, and TP).

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Selexipag Tablets
Ingredients	Active ingredient of this product: Selexipag Chemical name: 2-[4-[(5,6-diphenylpyrazin-2-yl)(2-propyl)amino)butylamino]-N-(methylsulfonyl)acetamide Molecular formula: C226H22N4O4S
Specifications	0.2mg*60 tablets

Registered Holders

BIOPHORE INDIA PHARMACEUTICALS PVT LTD

United States
Active
MSN LABORATORIES PRIVATE LTD

United States
Active
APOTEX PHARMACHEM INDIA PVT LTD

United States
Active

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